Which medications in the drug class Antineoplastic Agents are used in the treatment of Ovarian Cancer?

Updated: Aug 10, 2020
  • Author: Andrew E Green, MD; Chief Editor: Yukio Sonoda, MD  more...
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Antineoplastic Agents

Antineoplastic agents inhibit cell growth and proliferation. Several antineoplastic agents elicit a response in patients whose disease is resistant to platinum-based therapies. These include liposomal doxorubicin, topotecan, oral etoposide, gemcitabine, docetaxel, and vinorelbine. Other agents that may be used are ifosfamide, 5-fluorouracil with leucovorin, and altretamine (Hexalen).


Etoposide is a glycosidic derivative of podophyllotoxin that exerts its cytotoxic effect through stabilization of the normally transient covalent intermediates formed between DNA substrate and topoisomerase II, leading to single- and double-strand DNA breaks.

Topotecan (Hycamtin)

Topotecan binds to the topoisomerase I‑DNA complex and prevents religation of single-strand breaks.  Indicated as monotherapy for the treatment of patients with metastatic ovarian cancer after disease progression on or after initial or subsequent chemotherapy.

Gemcitabine (Gemzar)

Gemcitabine is a cytidine analog that is metabolized intracellularly to an active nucleotide. It inhibits ribonucleotide reductase and competes with deoxycytidine triphosphate for incorporation into DNA. It is indicated for advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy and is used in combination with carboplatin. It is cell-cycle specific for the S phase.

Docetaxel (Taxotere)

Docetaxel is a semisynthetic taxane, a class of drugs that inhibits cancer cell growth by promoting assembly and blocking the disassembly of microtubules, thereby preventing cancer cell division, leading to cell death.

Vinorelbine (Navelbine)

Vinorelbine is a semisynthetic vinca alkaloid that inhibits tubulin polymerization during G2 phase of cell division, thereby inhibiting mitosis.


Ifosfamide inhibits DNA and protein synthesis and, thus, cell proliferation, by causing DNA cross-linking and denaturation of double helix.

Fluorouracil (Adrucil)

Fluorouracil (5-FU) is a cycle-specific agent that has activity as single agent and, for many years, has been combined with biochemical modulator leucovorin. 5-FU inhibits tumor cell growth through at least 3 different mechanisms that ultimately disrupt DNA synthesis or cellular viability.

Melphalan (Alkeran)

Melphalan inhibits mitosis by cross-linking DNA strands. Tablets are indicated for the palliation of nonresectable epithelial ovarian carcinoma.

Altretamine (Hexalen)

The mechanism of action of altretamine is unclear; reactive intermediates covalently bind to microsomal proteins and DNA, possibly causing DNA damage. Altretamine inhibits DNA and RNA synthesis by inhibiting the incorporation of radioactive thymidine and uridine into DNA and RNA. Indicated as palliative treatment of patients with persistent or recurrent ovarian cancer.

Bevacizumab (Avastin)

Bevacizumab is a recombinant humanized monoclonal antibody to vascular endothelial growth factor (VEGF) receptors. Blocking the angiogenic VEGF receptor, in turn inhibits tumor angiogenesis, starving tumor of blood and nutrients. It is indicated in combination with paclitaxel, pegylated liposomal doxorubicin, or topotecan for platinum-resistant recurrent epithelial ovarian cancer in patients who received no more than 2 prior chemotherapy regimens. It is also indicated for women with platinum-sensitive recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer either in combination with carboplatin and paclitaxel or in combination with carboplatin and gemcitabine chemotherapy, followed by bevacizumab alone.

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